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PI3Kδ inhibitor

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  • Project profile
    Project name: PI3Kδ inhibitor
    Indications: Hematologic malignancies
    Research phase: Phase I, China; the patent has been granted in the US
    Cooperation demands: License-out and co-development
  • Highlights

    1. PI3Kδ selective inhibitor with a broad safety window

    (1) As an important member of the PI3K/mTOR pathway which regulates cell proliferation and cell cycle, PI3Kδ is involved in early signaling responses of leukocytes in a wide variety of stimulations.

    (2) PI3Kδ is only expressed in hematopoietic lineage, which remains a broad safety window for PI3Kδ selective inhibitors compared to pan-PI3K inhibitors or PI3Kα/β selective inhibitors.

    (3) High expression of PI3Kδ is found in Hematologic malignancies patients.

    2. A high selective inhibition of PI3Kδ in kinase and cellular level.

    Asset against PI3Kδ increased by 16 times at kinase levels and by 2–14 times at cellular levels compared with Idelalisib.

    3. Excellent anti-B cell activity and good safety in vivo.

    (1) Inhibition of asset on rat-activated B cells were 4-fold (1 h) and 15-fold (8 h) higher than that of Idelalisib, respectively, with less toxic than Idelalisib at the same dose in a 28-day repeated-dose toxicity test in rats.

    (2) hERG assay indicated the low risk of prolongation of QT interval and hERG block potency.

    (3) No genotoxicity was observed in the preclinical toxicity study. No abnormality was observed in the cardiovascular and respiratory systems when administered in species of SD Rats and Beagle Dogs.

    4. Clinical trial data: a suit for QD and a better AUC. (higher AUC than Idelalisib at a much lower dose)

    (1) t1/2 = 16.4 h at a dose of 25 mg, which is suitable for QD.

    (2) At the same dose, assets in humans showed a much higher AUC than Idelalisib.

  • Project Introduction

    1. Asset type: PI3Kδ inhibitor

    2. Indication: Hematologic malignancies

    3. Research phase: Phase I, China; the patent has been granted in the US

    4. Cooperation demands: License-out or co-development

    5. Research progress:

    (1) High selective PI3Kδ inhibitor on phase 1 trial.
    (2) No genotoxicity and no cardiovascular and respiratory system abnormality was observed in the pre-clinical study.
    (3) Good AUC was shown in clinical trial.

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